1-烷基-1-苄基-4-(3-氯-2-羟基)丙基哌嗪季铵盐的合成及生物活性

SYNTHESIS AND BIOLOGICAL ACTIVITIES OF 1-ALKYL-1-BENZYL-4-(3-CHLORO-2-HYDROXY)PROPYL PIPERAZINIUM HALIDES

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摘要设计合成了７个１烷基１苄基４（３氯２羟基）丙基哌嗪季铵盐（Ｉａ～ｇ）。生物活性试验结果表明，苄基苯环上连有强吸电子取代基时，可使抗炎和镇痛活性明显增强；季铵盐中的负离子对生物活性有一定的影响。在２０ｍｇ·ｋｇ－１的剂量下，Ｉｄ和Ｉｅ的抗炎活性和Ｉｅ的镇痛活性明显。 Seven 1alkyl1benzyl4(3chloro2hydroxy)propyl piperazinium halide hydrochloride were synthesized. Preliminary biological activity test showed that the presence of electroattracting group in the benzyl distinctly increased the analgesic and antiinflammatory activities of the compounds. For example, the analgesic activity of Ie and the antiinflammatory, activities of Id and Ie were all higher than those of Ia and Ib. The different anion of quaternary ammonium have some effect on the biological activity. However, this effect is not regular.

作者李润涛蔡俊超蔡孟深

机构地区北京医科大学药学院中国科学院上海药物研究所

出处《药学学报》 CAS CSCD 北大核心 1998年第1期28-33,共6页 Acta Pharmaceutica Sinica

关键词丙基哌嗪季铵盐抗炎镇痛 1Alkyl1benzyl4(3chloro2hydroxyl) propyl piperazinium halide Analgesic activity Antiinflammatory activity

分类号 TQ463.54 [化学工程—制药化工] R979.1 [医药卫生—药品]